DK2970225T3 - DIPEPTIDE AND TRIPEPTIDE AS EPOXY-KETONE PROTEASE INHIBITORS - Google Patents

DIPEPTIDE AND TRIPEPTIDE AS EPOXY-KETONE PROTEASE INHIBITORS Download PDF

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Publication number
DK2970225T3
DK2970225T3 DK14723553.5T DK14723553T DK2970225T3 DK 2970225 T3 DK2970225 T3 DK 2970225T3 DK 14723553 T DK14723553 T DK 14723553T DK 2970225 T3 DK2970225 T3 DK 2970225T3
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Prior art keywords
oxopropan
amino
mmol
methoxyphenyl
methyloxiran
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DK14723553.5T
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Danish (da)
English (en)
Inventor
Dustin Mcminn
Henry Johnson
David C Moebius
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Onyx Therapeutics Inc
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    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
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DK14723553.5T 2013-03-14 2014-03-14 DIPEPTIDE AND TRIPEPTIDE AS EPOXY-KETONE PROTEASE INHIBITORS DK2970225T3 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US201361786086P 2013-03-14 2013-03-14
US201361785608P 2013-03-14 2013-03-14
US201361847780P 2013-07-18 2013-07-18
US201361856847P 2013-07-22 2013-07-22
US201361883843P 2013-09-27 2013-09-27
US201361883798P 2013-09-27 2013-09-27
US201461941798P 2014-02-19 2014-02-19
PCT/US2014/026980 WO2014152127A1 (en) 2013-03-14 2014-03-14 Dipeptide and tripeptide epoxy ketone protease inhibitors

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DK2970225T3 true DK2970225T3 (en) 2018-09-24

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US (1) US9657057B2 (ru)
EP (1) EP2970225B1 (ru)
JP (2) JP2016515127A (ru)
KR (1) KR20150131276A (ru)
CN (1) CN105164117B (ru)
AU (2) AU2014240122B2 (ru)
BR (1) BR112015022856A8 (ru)
CA (1) CA2904085C (ru)
DK (1) DK2970225T3 (ru)
EA (1) EA030957B1 (ru)
ES (1) ES2687368T3 (ru)
IL (2) IL241180A0 (ru)
JO (1) JO3326B1 (ru)
MX (1) MX362489B (ru)
SG (1) SG11201507106PA (ru)
TW (1) TWI662047B (ru)
UY (1) UY35455A (ru)
WO (1) WO2014152127A1 (ru)

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KR102655020B1 (ko) 2016-06-29 2024-04-04 케자르 라이프 사이언스 펩티드 에폭시케톤 면역프로테아좀 억제제의 결정질 염
EA201990157A1 (ru) 2016-06-29 2019-05-31 Кезар Лайф Сайнсиз Способ получения пептидного эпоксикетонового ингибитора иммунопротеасомы и его предшественников
EP3318276A1 (en) 2016-11-04 2018-05-09 Janssen Biotech, Inc. Combinations of a telomerase inhibitor and a bcl-2 inhibitor for the treatment of hematological cancers
WO2018213263A1 (en) * 2017-05-15 2018-11-22 The Regents Of The University Of California Immunoproteasome inhibitor
CN107652219B (zh) 2017-08-14 2021-06-08 上海新理念生物医药科技有限公司 四马来酰亚胺型连接子及其应用
WO2019040680A1 (en) * 2017-08-23 2019-02-28 Krzar Life Sciences IMMUNOPROTEASOME INHIBITORS AND IMMUNOSUPPRESSANT AGENT IN THE TREATMENT OF AUTOIMMUNE DISORDERS
US20200276204A1 (en) 2017-09-21 2020-09-03 Kezar Life Sciences Combination therapy for immunological diseases
MX2020004936A (es) * 2017-11-16 2020-08-27 Amgen Inc Composiciones estables de compuestos de carfilzomib pegilado.
US10689416B2 (en) 2017-12-30 2020-06-23 Unity Biotechnology, Inc. Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer
EP3548504B1 (en) * 2017-12-30 2021-07-21 Unity Biotechnology, Inc. Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer
CN110092813B (zh) * 2019-06-05 2021-05-11 南京师范大学 一种三肽环氧丙烷衍生物及其制备方法和用途
CN118255835A (zh) * 2022-12-27 2024-06-28 上海美悦生物科技发展有限公司 三肽环氧酮化合物、药物组合物及其制备方法和用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5340736A (en) 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
US5858784A (en) 1991-12-17 1999-01-12 The Regents Of The University Of California Expression of cloned genes in the lung by aerosol- and liposome-based delivery
WO1998010779A1 (en) 1996-09-13 1998-03-19 New York University Method for treating parasitic diseases with proteasome inhibitors
US6042820A (en) 1996-12-20 2000-03-28 Connaught Laboratories Limited Biodegradable copolymer containing α-hydroxy acid and α-amino acid units
US6472375B1 (en) 1998-04-16 2002-10-29 John Wayne Cancer Institute DNA vaccine and methods for its use
DK1385870T3 (da) 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra hepatitis C-virus
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
DK2030981T3 (da) * 2004-05-10 2014-10-13 Onyx Therapeutics Inc Forbindelser til proteasom-enzymhæmning
DK1819353T3 (da) 2004-12-07 2011-05-16 Proteolix Inc Sammensætning til proteasomhæmning
US7589066B2 (en) * 2005-03-11 2009-09-15 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
PL1948678T3 (pl) * 2005-11-09 2013-09-30 Onyx Therapeutics Inc Związki do hamowania enzymów
DK2041158T3 (da) * 2006-06-19 2013-06-24 Onyx Therapeutics Inc Peptid-epoxidketoner til proteasom inhibering
EP2349313A4 (en) 2008-10-21 2012-08-29 Onyx Therapeutics Inc COMBINATION THERAPY WITH EPOXYCLETON PEPTIDES
MX2012010017A (es) * 2010-03-01 2012-10-01 Onyx Therapeutics Inc Compuestos de para la inhibicion de inmunoproteasomas.
US8455431B2 (en) * 2011-02-18 2013-06-04 Trustees of Dartmout College Inhibitors of the trypsin-like site of the proteasome and methods of use thereof
AR087863A1 (es) 2012-05-08 2014-04-23 Onyx Therapeutics Inc Procedimientos para la formacion de complejos de ciclodextrina para formular inhibidores del proteasoma peptidico

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